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Assay Detail

CHEMBL760598

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Binding
Inhibition of PDE4 enzyme from U937 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U-937
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Thalidomide analogs and PDE4 inhibition.
Muller GW, Shire MG, Wong LM, Corral LG, Patterson RT, Chen Y, Stirling DI.
Bioorg Med Chem Lett (1998) 8 : 2669 -2674
PubMed 9873600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.01 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313439 1 6.89
CHEMBL88475 1 6.64
CHEMBL315529 1 6.46
CHEMBL90349 1 6.13
CHEMBL88153 CDC-801 2.0 1 5.96
CHEMBL314759 1 5.89
CHEMBL90345 1 5.77
CHEMBL419135 1 5.70
CHEMBL88935 1 5.60
CHEMBL89890 1 5.03
CHEMBL468 THALIDOMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313439 IC50 = 130.0 nM 6.89
CHEMBL88475 IC50 = 230.0 nM 6.64
CHEMBL315529 IC50 = 350.0 nM 6.46
CHEMBL90349 IC50 = 740.0 nM 6.13
CHEMBL88153 CDC-801 IC50 = 1100.0 nM 5.96
CHEMBL314759 IC50 = 1300.0 nM 5.89
CHEMBL90345 IC50 = 1700.0 nM 5.77
CHEMBL419135 IC50 = 2000.0 nM 5.70
CHEMBL88935 IC50 = 2500.0 nM 5.60
CHEMBL89890 IC50 = 9400.0 nM 5.03
CHEMBL468 THALIDOMIDE IC50 > 500000.0 nM -